Rho

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抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S1314	Zoledronic Acid	<1 mg/mL	0.004 mg/mL	<1 mg/mL
S8031	NSC 23766	100 mg/mL	100 mg/mL	<1 mg/mL
S7319	EHop-016	<1 mg/mL	86 mg/mL	<1 mg/mL
S1721	Azathioprine	<1 mg/mL	54 mg/mL	<1 mg/mL
S7293	ZCL278	<1 mg/mL	100 mg/mL	<1 mg/mL
S8749	MBQ-167	<1 mg/mL	68 mg/mL	14 mg/mL
S5244	Zoledronic acid monohydrate	<1 mg/mL	0.01 mg/mL	<1 mg/mL
S7332	K-Ras(G12C) inhibitor 9	<1 mg/mL	53 mg/mL	<1 mg/mL
S7719	CCG-1423	<1 mg/mL	90 mg/mL	4 mg/mL
S8469	CCG-203971	<1 mg/mL	81 mg/mL	4 mg/mL
S7330	6H05	100 mg/mL	100 mg/mL	100 mg/mL
S7331	K-Ras(G12C) inhibitor 12	<1 mg/mL	27 mg/mL	<1 mg/mL
S8303	Kobe0065	<1 mg/mL	89 mg/mL	13 mg/mL
S7333	K-Ras(G12C) inhibitor 6	<1 mg/mL	81 mg/mL	30 mg/mL
S7607	BQU57	<1 mg/mL	66 mg/mL	20 mg/mL
S8499	KRpep-2d	100 mg/mL	-1 mg/mL	-1 mg/mL
S8156	ARS-853 (ARS853)	<1 mg/mL	86 mg/mL	1 mg/mL
S7482	EHT 1864 2HCl	100 mg/mL	100 mg/mL	<1 mg/mL
S7686	ML141	<1 mg/mL	81 mg/mL	<1 mg/mL

Rho抑制剂（20）
新Rho产品

产品目录	产品描述	文献引用	实验数据
S1314	Zoledronic Acid Zoledronic acid, 破骨细胞抑制剂，通过抑制甲羟戊酸途径诱导破骨细胞凋亡，并防止小GTP结合蛋白，如Ras 和 Rho的异戊二烯化。	Int J Cancer, 2016, 138(5):1281-9 Mol Cancer Ther, 2016, 15(5):854-65 J Mol Cell Cardiol, 2016, 99:76-86	Quantification (C) of SA-β-gal+ SMCs after sustained 100nM ADP treatment for 48hr with or without Ras inhibitor zoledronic acid (ZA) (n=4 in each group). #p<0.05, ##p<0.01 compared with control, p<0.05 compared with P2ry12+/+ADP. (D) Incidence of TAAD formation and rupture after BAPN administration with or without ZA. (E) Elastin degradation grades of mice aortas after BAPN administration with or without ZA. (F) Representative H&E staining of thoracic aorta and progression of thoracic aorta diameter of mice aortas after BAPN administration with or without ZA (n=8 in both group). (G) Representative images and quantification of SA-β-gal (blue) staining in mouse aorta after BAPN administration with or without ZA (n=4 in both group); arrow, location of SA-β-gal+ area. (H) Immunostaining and quantification of p-ERK and p-p38 in mouse aorta with or without ZA (n=4 in both group). Data are meanSD from three experiments.p<0.05, compared with no ZA.
S8031	NSC 23766 NSC 23766是一种Rac GTPase抑制剂，通过鸟嘌呤核苷酸因子(GEFs)靶向作用于Rac 活化，无细胞试验中IC50为~50 μM；但是不会抑制密切相关的靶点，Cdc42或RhoA。	Cancer Lett, 2016, 10.1016/j.canlet.2016.02.049 Sci Signal, 2018, 11(528) Cell Death Dis, 2015, 6:e1751	MES cells were treated with Rac inhibitor (50 μM EHT1864 or NSC23766) and assayed for self-renewal by serial passage mammosphere formation. P1, passage 1; P2, passage 2. Data are means ± SEM of three biological replicates. *P ≤ 0.05 by two-tailed t test.
S7319	EHop-016 EHop-016 是一种特异性Rac GTPase抑制剂，在MDA-MB-435 和 MDA-MB-231细胞中作用于Rac1，IC50为1.1 μM，同等有效抑制Rac3。	Cell Death Dis, 2015, 6:e1751 Biochem Pharmacol, 2016, 105:42-54	Human HCT116 cells were treated with conditioned media of (LPS + Chol)-treated THP-Ms or IL-1b (10 ng/ml) in the absence or presence of Ehop-016 (10 μM), and effects of the indicated factors on b-catenin transcriptional activity of HCT116 cells were determined by the TOP and FOP flash reporter assay, and the protein levels of GTP-Rac1, total Rac1, p-GSK3b (S9), total GSK3b, PCNA and Cyclin D1 were analyzed by western blot (H).
S1721	Azathioprine Azathioprine 是一种抑制免疫系统的药物，抑制了嘌呤的合成以及GTP结合蛋白Rac1的激活，用于器官移植和自身免疫性疾病。
S7293	ZCL278 ZCL278是一个选择性的Cdc42 GTP酶抑制剂，Kd为11.4 μM。	Cell Physiol Biochem, 2015, 36(4):1613-1627 Biol Trace Elem Res, 2016, 170(1):173-82	Rho GTPases were involved in NaAsO2 induced apoptosis in rat CGNs. A. Representative fluorescence images of cells exposed to 0 and 10 μM NaAsO2 for 24 h with or without ZCL278 (an inhibitor of Cdc42), or a Rac1 inhibitor NSC23766. Both ZCL278 and NSC23766 reduced the apoptotic cells. B. The graph indicates TUNEL-positive rat CGNs exposed to NaAsO2 (10 μM) with ZCL278 or NSC23766 groups decreased significantly compared with those of NaAsO2 treatment group. Data are expressed as mean ± SD from at least 5 visual fields. C. Rat CGNs in 96-well plates were treated by 0 and 10 μM NaAsO2 for 24h with or without ZCL278 (an inhibitor of Cdc42) pretreatment for 1 h, or a Rac1 inhibitor NSC23766 pretreatment for 12 h, and assessed by a CCK-8. ZCL278 and NSC23766 increased rat CGNs viability exposed to NaAsO2. All statistical results are expressed as means±SD from at least three independent experiments. ***P<0.001 vs control, # P<0.05, ##P<0.01, ###P<0.001 VS NaAsO2 treatment group.
S8749^New	MBQ-167 MBQ-167是一种有效的Rac和Cdc42双重抑制剂，在转移性乳腺癌细胞中，IC50分别为103 nM和78 nM。
S5244^New	Zoledronic acid monohydrate Zoledronic acid，一种含氮的二磷酸盐，是有效的破骨细胞抑制剂，可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。
S7332	K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 是致癌的K-Ras(G12C)的变构抑制剂。
S7684	Salirasib Salirasib是一种有效的竞争性_{prenylated protein methyltransferase (PPMTase)}抑制剂， K_i为2.6 μM，其抑制_Ras甲基化。Phase 2。
S7719	CCG-1423 CCG-1423是一种特定的 RhoA 通路抑制剂，能够抑制SRF介导的转录。	Cell Signal, 2017, 31:87-95	Cells were treated with CCG-1423 for 48 h. CCG-1423 blocked the nuclear translocation of MRTF-A.
S8469	CCG-203971 CCG-203971是一种新型的Rho/MRTF/SRF通路抑制剂，对SRE.L.的IC50值为0.64 μM。它可以抑制Rho介导的基因转录。
S7330	6H05 6H05是一个致癌K-Ras(G12C)的选择性、变构抑制剂。
S7331	K-Ras(G12C) inhibitor 12 K-Ras(G12C) inhibitor 12是致癌K-Ras(G12C)的变构抑制剂。	Oncotarget, 2016, 7(9):10064-72	(A) Proliferation of Calu-1 cells after SAHA and K-ras inhibitor (K-ras C12) treatment. Calu-1 cells, containing an activating G12C K-ras mutation, were treated with SAHA (2.5 mM) and K-ras C12 (10 mM) for 24 h and analyzed as in Figure Figure1A.1A. (B) Immunoblotting of Calu-1 cells treated with inhibitors. Cells were treated with inhibitors as indicated for 24 hrs. Cell lysates were collected and immunoblotted with antibodies indicated.
S8303	Kobe0065 Kobe0065是H-Ras-cRaf1相互作用的抑制剂，能有效抑制H-Ras·GTP与c-Raf-1 RBD的结合，Ki值为46±13 μM。
S7333	K-Ras(G12C) inhibitor 6 K-Ras(G12C) inhibitor 6 是一种变构的，选择性的致瘤性K-Ras(G12C)抑制剂。
S7607	BQU57 BQU57，RBC8的衍生物，是一种相对于GTPases Ras 和 RhoA的选择性GTPase Ral 抑制剂。
S8499	KRpep-2d KRpep-2d是选择性的K-Ras(G12D)抑制性环肽，相较于WT K-Ras和K-Ras(G12C)，对K-Ras(G12D)选择性更高，IC50为1.6 nM。
S8156	ARS-853 (ARS853) ARS-853是一种具有选择性的KRAS(G12C)共价结合抑制剂，通过结合GDP-肿瘤蛋白并阻止其激活，抑制突变型KRAS所驱动的信号通路。
S7482	EHT 1864 2HCl EHT 1864 2HCl是一种强效的Rac family GTPase抑制剂，其对Rac1, Rac1b, Rac2 和 Rac3的K_d分别为40 nM, 50 nM, 60 nM 和 250 nM 。	Mol Biol Cell, 2017, 28(13):1745-1753 Int J Clin Exp Pathol, 2016, 9(6):5902-5911	Inhibition of Rac1 activity by EHT 1864 blocks alignment under flow, whereas solvent control-treated ECs aligned in the direction of flow. Note that the inhibitor was present throughout the experiment, due to the closed system that is used for long-term flow experiments. Bar graph on the right shows percentage of aligned cells in under static and flow conditions for both EHT 1864-treated and solvent-treated Ctrl ECs. ECs orientated between a 0-45° angle are quantified as being aligned. Data are mean of three independent experiments ± SEM. ***P<0.001. Bar, 25μm.
S7686	ML141 ML141是Rho家族GTPase cdc42的一种有效的，选择性可逆非竞争性抑制剂，IC50为200 nM。对cdc42比对其他Rho家族中的GTPases(如Rac1, Rab2, Rab7)更有选择性。		(A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.

研究领域

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Rho

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研究领域